The study of adrenal function began back in XIX century, but only in 1936 from extracts of the adrenal cortex at the same time Kendall and Wintersteiner in USA and Reinstein in Switzerland allocated steroids to crystalline form.
At 1948 cortisone was obtained in sufficient for clinical trials, and in further – hydrocortisone. Today there is a wide range of synthetic glucocorticosteroids ( Corticosteroid ) used in clinical practice.
In the synthesis of new Corticosteroid efforts were directed at creating drugs with more selective action than hydrocortisone. It was possible to achieve a significant reduction in the mineralocorticoid activity of synthetic corticosteroids. For example, prednisone is almost devoid ofmineralocorticoid properties.
By The chemical structure of prednisolone is a modified hydrocortisone molecule, in which introduced a double bond between the 1st and 2 atoms of the steroid nucleus, which reduced mineralocorticoid activity and, in addition, significantly increase its anti-inflammatory activity. Thus, a small structural change caused a significant increase in the biological activity of the hormone.
Corticosteroid applied in medical practice in mostly in as anti-inflammatory, anti-shock, anti-allergic agents and immunosuppressant’s.
Corticosteroid, in particular prednisone have a versatile effect on organism, regulate protein and fat metabolism affect carbohydrate metabolism.
Prednisolone regulates insulin synthesis and glucagon stimulates gluconeogenesis by inducing its regulating enzymes, increases the glycogen content in liver, stimulating the activity of glycogen synthase, inhibits glucose uptake by lipocytes, stimulating lipolysis.
Corticosteroid have a catabolic effect and may cause dystrophic changes in lymphoid and connective tissue, muscle, subcutaneous and adipose tissue and skin.
The mechanism of anti-inflammatory action of Corticosteroid associated with their influence on quantity, distribution and leukocyte function. After a single injection of prednisone in peripheral tissue decreases the number of T- and B-lymphocytes, monocytes, eosinophilic and basophilic granulocytes, while the content of neutrophilic granulocytes increases. This is due to two factors: increased neutrophil granulocyte intake from the bone marrow and decrease in migration from the blood, which leads to reduce their number in focus of inflammation. Decrease in peripheral blood counts of lymphocytes, monocytes, eosinophilic and basophilic granulocytes is a consequence of their transition from the blood into lymphoid tissue.
Prednisolone inhibits the function of leukocytes and tissue macrophages. Its impact on tissue macrophages lies in limiting their ability to phagocytosis, as well as to production of pyrogens, collagenase, elastase and plasminogen activators. Inhibiting the function of leukocytes, prednisone can affect and on other mechanisms of inflammation: decreases capillary permeability, inhibiting the activity of inhibits the release of histamine from mast cells.
The immunosuppressive effect of prednisone is due, in addition to the effect on migration and interaction T- and B lymphocytes, exposure to the complement system as well as the inhibition of products and effects of interleukin-2.
Prednisolone has anti-shock, anti-allergic, anti-inflammatory effect. With prolonged use inhibits the synthesis and ACTH secretion by the pituitary gland and secondary secretion of Corticosteroid adrenal glands.
After intravenous administration, prednisone binds to blood plasma globulin – transcortin. The maximum concentration of free prednisone in blood plasma is reached 10 minutes after intravenous and 60 minutes after intramuscular injection.
Prednisolone is a corticosteroid average duration of action. The half-life is about 3 hours. Actively metabolized during many tissues, especially intensely in liver, displayed in as metabolites, predominantly with urine.
Prednisone is shown:
- As an agent for emergency care in case of burn, traumatic, transfusion , and infectious-toxic shock;
- at endocrinology – with primary or secondary adrenal insufficiency, in including acute; purulent thyroiditis ;
- at rheumatology and therapies for rheumatoid arthritis and systemic lupus erythematosus;
- at dermatology – with severe polymorphic erythema, exfoliative dermatitis;
- In severe allergic diseases resistant to adequate therapy with antihistamines, contact and atopic dermatitis, serum sickness, drug allergies, transfusion reactions, asthmatic status, acute laryngeal edema of non-infectious etiology;
- at hematology – with idiopathic thrombocytopenic purpura, acute and chronic leukemia;
- at neurology – with multiple sclerosis;
- at transplantation – to suppress the graft rejection reaction;
- at infectious diseases clinic – toxic shock (with simultaneous antibiotic therapy);
- at pediatrics – allergic reactions, in including anaphylaxis; laryngitis, laryngotracheitis; severe forms of bronchial asthma, asthmatic status.
For shock, prednisolone is administered intravenously slowly or intravenously in a dose of 30–90 mg. For other indications – 30–45 mg intravenously slowly. If intravenous drug administration is difficult, then it can be administered deep intramuscularly.
Side effects and contraindications to the use of prednisone is the same as for other Corticosteroid intended for systemic corticosteroid therapy.
The widespread introduction of prednisone, especially injectable dosage forms, into medical practice was saved not by one human life. Along with new and active corticosteroid Prednisolone is effective, proven and affordable drug, topical and at present tense
What you need to know when taking this drug
Most often in non-medical circles it is called a steroid or glucocorticoid , many people think that it is a very dangerous drug and with great reluctance agree to be treated with this drug.
But for certain diseases, it is prednisone that is considered mandatory and necessary drug of first choice in the treatment of disease.
It will not be about the drug itself and under what diseases it should be prescribed, but our information block that doctors usually forget when prescribing prednisone. Usually, children come to the consultation while taking prednisone in combination with asparkam . Believe me, hypokalemia(decrease in the level of potassium in the blood) in connection with which prescribe asparkam is not the most common complication in the appointment of prednisone.
In our practice, the departments of almost 90% of patients receiving this drug are observed with a diagnosis of nephrotic syndrome.
Prednisolone is prescribed for a long time (a full course of therapy until the drug can be discontinued may last 6-12 months), you must prescribe additional drugs to prevent the side effects of prednisone. It:
- In order to protect the mucous membrane of the upper gastrointestinal tract (esophagus, stomach, duodenum), prednisolone may cause indigestion, nausea, vomiting and more serious complications like steroid ulcers. However, all this can be avoided by taking the so-called -gastroprotective drugs (ie the protection of the stomach in literal translation). These are antacid drugs (for example, Maalox, phosphalugel , etc.), H + pump blockers (for example, Omeprazole ), drugs that improve the motility of the gastrointestinal tract. All doses of drugs are selected individually according to age and body weight.
- Bone protection. Prolonged use of steroids can cause a decrease in bone mass, so-called steroid osteoporosis (bone loss) can develop , which ultimately leads to bone fractures. But this condition can also be prevented, it is necessary to take calcium and vitamin D preparations . The dose of drugs is also selected individually.
What else you need to pay attention to:
- It is mandatory to monitor blood pressure
- Observation by an ophthalmologist: vision control, the state of intraocular pressure and the lens of the eye.
- For very long-term use of prednisone, check blood glucose levels.
- The state of mental health. Children often become capricious, sometimes even aggressive. This condition passes independently after discontinuation of the drug.
- Watch for weight and diet. On the background of taking prednisone, appetite is greatly increased. However, as a parent, you can control the nutrition of your child, it is necessary to limit the intake of easily digestible carbohydrates.
- In order to monitor and evaluate the effectiveness of gastroprotective therapy, the mucous membrane of the upper gastrointestinal tract is evaluated by – endoscopy (gastroscopy).
This information was prepared by an employee of the department (pediatrician) for informational purposes. Be sure to consult with your doctor.